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Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 01; Vol. 18 (1), pp. 28-33. Date of Electronic Publication: 2007 Nov 13. - Publication Year :
- 2008
-
Abstract
- Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activities and encouraging oral pharmacokinetic profiles.
- Subjects :
- Animals
Anticoagulants chemistry
Anticoagulants pharmacokinetics
Anticoagulants pharmacology
Bridged Bicyclo Compounds, Heterocyclic pharmacokinetics
Bridged Bicyclo Compounds, Heterocyclic pharmacology
Hydrophobic and Hydrophilic Interactions
Male
Models, Molecular
Pyrrolidinones pharmacokinetics
Pyrrolidinones pharmacology
Rats
Rats, Sprague-Dawley
Serine Proteinase Inhibitors pharmacokinetics
Serine Proteinase Inhibitors pharmacology
Stereoisomerism
Structure-Activity Relationship
Bridged Bicyclo Compounds, Heterocyclic chemistry
Factor Xa Inhibitors
Pyrrolidinones chemistry
Serine Proteinase Inhibitors chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18053714
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.11.019